CN102574812B - 新型苯并咪唑衍生物及它们作为fxr激动剂的用途 - Google Patents

新型苯并咪唑衍生物及它们作为fxr激动剂的用途 Download PDF

Info

Publication number
CN102574812B
CN102574812B CN201080043283.8A CN201080043283A CN102574812B CN 102574812 B CN102574812 B CN 102574812B CN 201080043283 A CN201080043283 A CN 201080043283A CN 102574812 B CN102574812 B CN 102574812B
Authority
CN
China
Prior art keywords
difluoro
phenyl
chloro
benzimidazole
benzimidazol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN201080043283.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN102574812A (zh
Inventor
格雷戈里·马丁·本森
康拉德·辈莱切
冯松
尤伟·格雷瑟
贝恩德·库恩
勒内·E·马丁
让-马克·普朗谢
汉斯·里斯特
马库斯·鲁道夫
斯文·泰勒
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CN102574812A publication Critical patent/CN102574812A/zh
Application granted granted Critical
Publication of CN102574812B publication Critical patent/CN102574812B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201080043283.8A 2009-09-29 2010-09-27 新型苯并咪唑衍生物及它们作为fxr激动剂的用途 Expired - Fee Related CN102574812B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09171700.9 2009-09-29
EP09171700 2009-09-29
PCT/EP2010/064217 WO2011039130A1 (en) 2009-09-29 2010-09-27 New benzimidazole derivatives and their use as fxr agonists

Publications (2)

Publication Number Publication Date
CN102574812A CN102574812A (zh) 2012-07-11
CN102574812B true CN102574812B (zh) 2016-03-30

Family

ID=43033176

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080043283.8A Expired - Fee Related CN102574812B (zh) 2009-09-29 2010-09-27 新型苯并咪唑衍生物及它们作为fxr激动剂的用途

Country Status (12)

Country Link
US (1) US8309581B2 (enExample)
EP (1) EP2483247A1 (enExample)
JP (1) JP5503007B2 (enExample)
KR (1) KR101477872B1 (enExample)
CN (1) CN102574812B (enExample)
AU (1) AU2010303146A1 (enExample)
BR (1) BR112012006986A2 (enExample)
CA (1) CA2772815A1 (enExample)
IL (1) IL218037A0 (enExample)
IN (1) IN2012DN01234A (enExample)
MX (1) MX2012002479A (enExample)
WO (1) WO2011039130A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3043865T (pt) 2013-09-11 2021-01-14 Univ Claude Bernard Lyon Métodos e composições farmacêuticas para o tratamento da infeção por vírus da hepatite b
CN108072684B (zh) * 2016-11-11 2020-06-16 中国科学院广州生物医药与健康研究院 法尼醇x受体的新配体及其筛选方法和应用
KR20190117632A (ko) 2017-02-21 2019-10-16 장피트 Ppar 효현제와 fxr 효현제의 병용
JP2020515564A (ja) 2017-03-30 2020-05-28 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101228152A (zh) * 2005-07-22 2008-07-23 赛诺菲-安万特 N-(杂芳基)-1-杂芳基烷基-1h-吲哚-2-羧基酰胺衍生物、其制备方法及其在制药中的应用
WO2008101586A1 (de) * 2007-02-21 2008-08-28 Merck Patent Gmbh Benzimidazolderivate
CN101479249A (zh) * 2006-06-29 2009-07-08 霍夫曼-拉罗奇有限公司 苯并咪唑衍生物、其制备方法、它们作为fxr激动剂的用途及含有它们的药物制剂

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2188263B1 (en) * 2007-08-27 2012-06-27 F. Hoffmann-La Roche AG Benzimidazole derivatives used as fxr agonists
AU2008323017B2 (en) * 2007-11-15 2012-12-20 F. Hoffmann-La Roche Ag Methyl-benzimidazole derivatives
ES2407180T3 (es) * 2008-09-11 2013-06-12 F. Hoffmann-La Roche Ag Nuevos derivados de bencimidazol
AU2009304169A1 (en) * 2008-10-15 2010-04-22 F. Hoffmann-La Roche Ag New benzimidazole derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101228152A (zh) * 2005-07-22 2008-07-23 赛诺菲-安万特 N-(杂芳基)-1-杂芳基烷基-1h-吲哚-2-羧基酰胺衍生物、其制备方法及其在制药中的应用
CN101479249A (zh) * 2006-06-29 2009-07-08 霍夫曼-拉罗奇有限公司 苯并咪唑衍生物、其制备方法、它们作为fxr激动剂的用途及含有它们的药物制剂
WO2008101586A1 (de) * 2007-02-21 2008-08-28 Merck Patent Gmbh Benzimidazolderivate

Also Published As

Publication number Publication date
AU2010303146A1 (en) 2012-04-19
MX2012002479A (es) 2012-03-26
CA2772815A1 (en) 2011-04-07
KR20120063536A (ko) 2012-06-15
US20110077273A1 (en) 2011-03-31
HK1171746A1 (zh) 2013-04-05
CN102574812A (zh) 2012-07-11
JP5503007B2 (ja) 2014-05-28
US8309581B2 (en) 2012-11-13
WO2011039130A1 (en) 2011-04-07
EP2483247A1 (en) 2012-08-08
IN2012DN01234A (enExample) 2015-05-15
BR112012006986A2 (pt) 2016-04-12
KR101477872B1 (ko) 2014-12-30
JP2013505977A (ja) 2013-02-21
IL218037A0 (en) 2012-04-30

Similar Documents

Publication Publication Date Title
CN101772487B (zh) 甲状腺类化合物
CN102164899B (zh) 用作抗异常脂肪血症及相关疾病的fxr调节剂的取代的吲唑或四氢吲唑类
CN102149688B (zh) 新型苯并咪唑衍生物
TW200936576A (en) Carboxyl-or hydroxylsubstituted benzimidazole derivatives
TW200811112A (en) Benzimidazole derivatives
KR20020087382A (ko) 진성 당뇨병 치료를 위한 벤조산 유도체
CN105431416A (zh) 4-炔基咪唑衍生物和含有其作为有效成分的药物
CN102574812B (zh) 新型苯并咪唑衍生物及它们作为fxr激动剂的用途
TW200924755A (en) Novel methyl-benzimidazole derivatives
KR20110069173A (ko) 신규한 벤즈이미다졸 유도체
HK1171746B (en) New benzimidazole derivatives and their use as fxr agonists
CN102791695B (zh) 作为fxr调节剂的环戊基-和环庚基吡唑类
HK1221215B (zh) 4-炔基咪唑衍生物和含有其作为有效成分的药物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1171746

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1171746

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160330

Termination date: 20180927